| 品牌 | 货号 | 产品规格 | 价格(RMB) | 库存（上海） | 北京 | 武汉 | 南京 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
| 源叶(MedMol) | S81732-10mg | 99% | ￥410.00元 | 预计交期：2-3天 | - | - | - |
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| 源叶(MedMol) | S81732-50mg | 99% | ￥880.00元 | 预计交期：2-3天 | - | - | - |
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| 源叶(MedMol) | S81732-100mg | 99% | ￥1400.00元 | 预计交期：2-3天 | - | - | - |
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| 源叶(MedMol) | S81732-500mg | 99% | ￥3900.00元 | 预计交期：2-3天 | - | - | - |
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| 产品描述： Dactolisib Tosylate (BEZ235 Tosylate) is a dual PI3K and mTOR kinase inhibitor with IC50 values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively. Dactolisib Tosylate (BEZ235 Tosylate) inhibits mTORC1 and mTORC2 | ||||||||||||||||||||
| 靶点： p110α：4 nM (IC50)；p110α-H1047R：4.6 nM (IC50)；p110α-E545K：5.7 nM (IC50)；p110γ：5 nM (IC50)；p110δ；7 nM (IC50)；p110β：75 nM (IC50)；mTOR：20.7 nM (IC50)；mTORC1；mTORC2；Autophagy;PI3K; mTOR | ||||||||||||||||||||
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体外研究： Dactolisib (BEZ235) is an imidazo[4,5-c]quinoline derivative that inhibits PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these enzymes. The IC50s for PI3Kα, β, γ, δ are 4, 75, 7, 5 nM, respectively. It is also found to be as active against the mutant PI3KαE545K or PI3KαH1047R with IC50s of 5.7 and 4.6 nM, respectively. In human tumor cell lines, it is able to effectively and specifically block the dysfunctional activation of the PI3K pathway, inducing G1 arrest. PTEN-null cell lines PC3M and U87MG shows a dose-dependent reduction in cell proliferation when treated with increasing concentrations of Dactolisib (BEZ235), with an average GI50 of 10 to 12 nM |
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体内研究： Dactolisib (BEZ235) is well tolerated, displays disease stasis when administered orally, and enhances the efficacy of other anticancer agents. At a dose of 50 mg/kg, Dactolisib (BEZ235) appears rapidly in plasma with a Cmax of 1.68 μM at 0.5 h and a C24h of 0.03 μM |
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参考文献： 1. Maira SM, et al. Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity. Mol Cancer Ther, 2008, 7(7), 1851-1863. |
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| 溶解性： soluble in DMSO | ||||||||||||||||||||
| 保存条件： -20℃ | ||||||||||||||||||||
配置溶液浓度参考：
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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